期刊
BIOORGANIC CHEMISTRY
卷 56, 期 -, 页码 34-40出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2014.05.009
关键词
Hepatocellular carcinoma; MTS derivatives; Synthesis; Anti-tumor activity
资金
- National Natural Science Foundation of China [30760292, 81302808]
- Research Council of The University of Hong Kong [104002320]
- Wong's Donation for Modern Oncology of Chinese Medicine [200006276]
- Science and Technology Department of Guizhou Province [QKHZYZ [2012] 5054, QKHZYZ [2010]5018]
- Ministry of Science and Technology of China [2011ZX09102-009-02]
A series of Matijin-Su (MTS, N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol) derivatives was synthesized and evaluated for their anti-tumor activities in hepatocellular carcinoma cells. The IC50 of compounds 1, 3, 4, 11, 13 were less than 20 mu M, and compound 1 and 3 showed an IC50 value of less than 9 mu M. Expansion inhibition could be found significantly in compound 1 and 3-treated human hepatoma cell HepG2 and PLC/PRF/5, while both compounds exhibit lower toxicity to human hepatocyte cell line L-02. Compound 1 and 3 could induce cell cycle arrest at G1/S phase. This may be attributed to increase level of intracellular reactive oxygen species (ROS). Up-regulation of p38 MAPK activity in responding the ROS stabilize p53 and activate p21 transcription, the critical regulatory in G1/S checkpoint. Observations in this study shed light on the potential of MTS derivatives compound 1 and 3 as novel suppressors to human liver cancer. (C) 2014 Elsevier Inc. All rights reserved.
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